Cargando…

Synthesis of substituted 15β-alkoxy estrone derivatives and their cofactor-dependent inhibitory effect on 17β-HSD1

17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a key enzyme in the biosynthesis of 17β-estradiol. Novel estrone-based compounds bearing various 15β-oxa-linked substituents and hydroxy, methoxy, benzyloxy, and sulfamate groups in position C3 as potential 17β-HSD1 inhibitors have been synthesiz...

Descripción completa

Detalles Bibliográficos
Autores principales:	Herman, Bianka Edina, Kiss, Anita, Wölfling, János, Mernyák, Erzsébet, Szécsi, Mihály, Schneider, Gyula
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Taylor & Francis 2019
Materias:	Research Paper
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6691805/ https://www.ncbi.nlm.nih.gov/pubmed/31307240 http://dx.doi.org/10.1080/14756366.2019.1634064

Ejemplares similares

Synthesis of novel 13α-estrone derivatives by Sonogashira coupling as potential 17β-HSD1 inhibitors
por: Bacsa, Ildikó, et al.
Publicado: (2017)

Synthesis and Biological Evaluation of Triazolyl 13α-Estrone–Nucleoside Bioconjugates
por: Bodnár, Brigitta, et al.
Publicado: (2016)

Synthesis and structure–activity relationships of 2- and/or 4-halogenated 13β- and 13α-estrone derivatives as enzyme inhibitors of estrogen biosynthesis
por: Bacsa, Ildikó, et al.
Publicado: (2018)

Pd-Catalyzed microwave-assisted synthesis of phosphonated 13α-estrones as potential OATP2B1, 17β-HSD1 and/or STS inhibitors
por: Jójárt, Rebeka, et al.
Publicado: (2018)

The first Pd-catalyzed Buchwald–Hartwig aminations at C-2 or C-4 in the estrone series
por: Bacsa, Ildikó, et al.
Publicado: (2018)

β-Amino- and Alkoxy-Substituted Disilanides
por: Balatoni, Istvan, et al.
Publicado: (2019)

Antiproliferative and Antimetastatic Properties of 16-Azidomethyl Substituted 3-O-Benzyl Estrone Analogs †
por: Senobar Tahaei, Seyyed Ashkan, et al.
Publicado: (2023)

Synthesis of Novel C-2- or C-15-Labeled BODIPY—Estrone Conjugates
por: Bacsa, Ildikó, et al.
Publicado: (2018)

Microwave-Assisted Stereoselective Heterocyclization to Novel Ring d-fused Arylpyrazolines in the Estrone Series
por: Mótyán, Gergő, et al.
Publicado: (2019)

Synthesis, Biological Evaluation and Docking Studies of 13-Epimeric 10-fluoro- and 10-Chloroestra-1,4-dien-3-ones as Potential Aromatase Inhibitors
por: Jójárt, Rebeka, et al.
Publicado: (2019)

A molecular understanding of d-homoestrone-induced G2/M cell cycle arrest in HeLa human cervical carcinoma cells
por: Minorics, Renáta, et al.
Publicado: (2015)

Synthesis and in Vitro Antiproliferative Evaluation of C-13 Epimers of Triazolyl-d-Secoestrone Alcohols: The First Potent 13α-d-Secoestrone Derivative
por: Szabó, Johanna, et al.
Publicado: (2016)

Eugenol β-Amino/β-Alkoxy Alcohols with Selective Anticancer Activity
por: Teixeira, Cláudia, et al.
Publicado: (2022)

Chemical Synthesis and Biological Evaluation of 3-Substituted Estrone/Estradiol Derivatives as 17β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors Acting via a Reverse Orientation of the Natural Substrate Estrone
por: Ngueta, Adrien Djiemeny, et al.
Publicado: (2023)

Copper-catalyzed reactions of β-alkoxy/phenoxy enones with dimethyl diazomalonate
por: GÜNGÖR, Füsun Şeyma
Publicado: (2022)

Investigation of the Antineoplastic Effects of 2-(4-Chlorophenyl)-13α-Estrone Sulfamate against the HPV16-Positive Human Invasive Cervical Carcinoma Cell Line SiHa
por: Ali, Hazhmat, et al.
Publicado: (2023)

Impact of Substitution Pattern and Chain Length on the Thermotropic Properties of Alkoxy-Substituted Triphenyl-Tristriazolotriazines †
por: Rieth, Thorsten, et al.
Publicado: (2020)

Synthesis of Novel 2-(Isopropylamino)thiazol-4(5H)-one Derivatives and Their Inhibitory Activity of 11β-HSD1 and 11β-HSD2 in Aspect of Carcinogenesis Prevention
por: Kupczyk, Daria, et al.
Publicado: (2020)

The Influence of Alkoxy Substitutions on the Properties of Diketopyrrolopyrrole-Phenyl Copolymers for Solar Cells
por: George, Zandra, et al.
Publicado: (2013)

Bent and Twisted: Synthesis of an Alkoxy-Substituted (1,5)Naphthalene-paracyclophanediene
por: Mann, Arielle, et al.
Publicado: (2023)

Copper-Catalyzed Oxidative Cleavage of the C–C Bonds of β-Alkoxy Alcohols and β-1 Compounds
por: Kim, Si Ae, et al.
Publicado: (2020)

Inhibitory Effects of Prunella vulgaris L. Extract on 11β-HSD1 in Human Skin Cells
por: Roh, Kyung-Baeg, et al.
Publicado: (2018)

Receptor Interaction Profiles of 4-Alkoxy-Substituted 2,5-Dimethoxyphenethylamines and Related Amphetamines
por: Kolaczynska, Karolina E., et al.
Publicado: (2019)

Estrone and 17β‐Estradiol Reverse Breast Cancer Resistance Protein‐mediated Multidrug Resistance
por: Imai, Yasuo, et al.
Publicado: (2002)

11β-HSD Types 1 and 2 in the Songbird Brain
por: Rensel, Michelle A., et al.
Publicado: (2018)

Synthesis, opioid receptor binding profile and SAR studies of 14-alkoxy-substituted indolo- and benzofuromorphinans
por: Staaf, Alexander, et al.
Publicado: (2008)

Synthesis and Hydrogen‐Bond Patterns of Aryl‐Group Substituted Silanediols and ‐triols from Alkoxy‐ and Chlorosilanes
por: Kannengießer, Jan‐Falk, et al.
Publicado: (2021)

The Flögel-three-component reaction with dicarboxylic acids – an approach to bis(β-alkoxy-β-ketoenamides) for the synthesis of complex pyridine and pyrimidine derivatives
por: Bera, Mrinal K, et al.
Publicado: (2014)

Yeast-based assays for screening 11β-HSD1 inhibitors
por: Vanella, Rosario, et al.
Publicado: (2016)

Macrophage 11β-HSD-1 deficiency promotes inflammatory angiogenesis
por: Zhang, Zhenguang, et al.
Publicado: (2017)

11β-HSD as a New Target in Pharmacotherapy of Metabolic Diseases
por: Kupczyk, Daria, et al.
Publicado: (2022)

The Role of Estrone in Feminizing Hormone Treatment
por: Tebbens, Marieke, et al.
Publicado: (2021)

11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors Still Improve Metabolic Phenotype in Male 11β-HSD1 Knockout Mice Suggesting Off-Target Mechanisms
por: Harno, Erika, et al.
Publicado: (2013)

Synthesis of β-alkoxy-N-protected phenethylamines via one-pot copper-catalyzed aziridination and ring opening
por: Saavedra-Olavarría, Jorge, et al.
Publicado: (2018)

Biological, pharmacological and immunological activities of novel 6-amino-acid-substituted 14-alkoxy-N-methylmorphinans
por: Guerrieri, Elena, et al.
Publicado: (2011)

Design, sythesis and evaluation of a series of 3- or 4-alkoxy substituted phenoxy derivatives as PPARs agonists
por: Zhang, Jun, et al.
Publicado: (2017)

Synthesis and Molecular Docking Studies of Alkoxy- and Imidazole-Substituted Xanthones as α-Amylase and α-Glucosidase Inhibitors
por: Aguila-Muñoz, Dolores G., et al.
Publicado: (2023)

Single and Competitive Adsorption of 17α-Ethinylestradiol and Bisphenol A with Estrone, β-Estradiol, and Estriol onto Sediment
por: Li, Yu, et al.
Publicado: (2014)

Novel Indoline Spiropyrans Based on Human Hormones β-Estradiol and Estrone: Synthesis, Structure, Chromogenic and Cytotoxic Properties
por: Ozhogin, Ilya V., et al.
Publicado: (2023)

Antiproliferative Properties of Newly Synthesized 19-Nortestosterone Analogs Without Substantial Androgenic Activity
por: Gyovai, András, et al.
Publicado: (2018)

Cannot write session to /tmp/vufind_sessions/sess_hoqvk9cu4km6ihiurfuokh3s19